JP2005524730A5 - - Google Patents
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- Publication number
- JP2005524730A5 JP2005524730A5 JP2004501483A JP2004501483A JP2005524730A5 JP 2005524730 A5 JP2005524730 A5 JP 2005524730A5 JP 2004501483 A JP2004501483 A JP 2004501483A JP 2004501483 A JP2004501483 A JP 2004501483A JP 2005524730 A5 JP2005524730 A5 JP 2005524730A5
- Authority
- JP
- Japan
- Prior art keywords
- diblock copolymer
- valerolactone
- polymer
- dosage form
- polymer block
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 229920000359 diblock copolymer Polymers 0.000 claims 21
- 229920000642 polymer Polymers 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 12
- 239000002552 dosage form Substances 0.000 claims 10
- AEMRFAOFKBGASW-UHFFFAOYSA-N glycolic acid Chemical group OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 10
- YFHICDDUDORKJB-UHFFFAOYSA-N Trimethylene carbonate Chemical group O=C1OCCCO1 YFHICDDUDORKJB-UHFFFAOYSA-N 0.000 claims 9
- 239000000178 monomer Substances 0.000 claims 8
- PAPBSGBWRJIAAV-UHFFFAOYSA-N ε-caprolactone Chemical group O=C1CCCCCO1 PAPBSGBWRJIAAV-UHFFFAOYSA-N 0.000 claims 8
- VKSWWACDZPRJAP-UHFFFAOYSA-N 1,3-dioxepan-2-one Chemical group O=C1OCCCCO1 VKSWWACDZPRJAP-UHFFFAOYSA-N 0.000 claims 7
- VPVXHAANQNHFSF-UHFFFAOYSA-N 1,4-dioxan-2-one Chemical group O=C1COCCO1 VPVXHAANQNHFSF-UHFFFAOYSA-N 0.000 claims 7
- 229960000380 Propiolactone Drugs 0.000 claims 7
- VEZXCJBBBCKRPI-UHFFFAOYSA-N β-Propiolactone Chemical group O=C1CCO1 VEZXCJBBBCKRPI-UHFFFAOYSA-N 0.000 claims 7
- YEJRWHAVMIAJKC-UHFFFAOYSA-N γ-lactone 4-hydroxy-butyric acid Chemical group O=C1CCCO1 YEJRWHAVMIAJKC-UHFFFAOYSA-N 0.000 claims 7
- OZJPLYNZGCXSJM-UHFFFAOYSA-N δ-Valerolactone Chemical group O=C1CCCCO1 OZJPLYNZGCXSJM-UHFFFAOYSA-N 0.000 claims 7
- 239000004480 active ingredient Substances 0.000 claims 5
- 239000007788 liquid Substances 0.000 claims 5
- 229920001223 polyethylene glycol Polymers 0.000 claims 4
- GAEKPEKOJKCEMS-UHFFFAOYSA-N γ-Valerolactone Chemical group CC1CCC(=O)O1 GAEKPEKOJKCEMS-UHFFFAOYSA-N 0.000 claims 4
- 239000007864 aqueous solution Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- 229920001477 hydrophilic polymer Polymers 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000007911 parenteral administration Methods 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 238000003756 stirring Methods 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- AOLNDUQWRUPYGE-UHFFFAOYSA-N 1,4-dioxepan-5-one Chemical compound O=C1CCOCCO1 AOLNDUQWRUPYGE-UHFFFAOYSA-N 0.000 claims 1
- LCGLNKUTAGEVQW-UHFFFAOYSA-N dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 claims 1
- 238000002156 mixing Methods 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
Claims (27)
[式中、
ポリマーブロックAは、<1,000の分子量を有する線状の製薬学的に許容され得る親水性ポリマーを示し、
ポリマーブロックBは、グリコール酸、プロピオラクトン、γ−ブチロラクトン、δ−バレロラクトン、γ−バレロラクトン、ε−カプロラクトン、トリメチレンカーボネート、p−ジオキサノン、テトラメチレンカーボネート、ε−ラクトン、1,5−ジオキセパン−2−オンから選ばれる少なくとも2種のモノマーを含んでなるポリマーを示す]
のジブロックコポリマーであって、ジブロックコポリマーが50℃より低い温度で液体であることを特徴とするジブロックコポリマー。 Formula AB
[Where:
Polymer block A represents a linear pharmaceutically acceptable hydrophilic polymer having a molecular weight of <1,000,
Polymer block B is glycolic acid, propiolactone, γ-butyrolactone, δ-valerolactone, γ-valerolactone, ε-caprolactone, trimethylene carbonate, p-dioxanone, tetramethylene carbonate, ε-lactone, 1,5- Indicates a polymer comprising at least two monomers selected from dioxepane-2-one]
A diblock copolymer according to claim 1, wherein the diblock copolymer is a liquid at a temperature lower than 50 ° C.
[式中、[Where:
ポリマーブロックAは、<1,000の分子量を有する線状の製薬学的に許容され得る親水性ポリマーを示し、Polymer block A represents a linear pharmaceutically acceptable hydrophilic polymer having a molecular weight of <1,000,
ポリマーブロックBは、トリメチレンカーボネートのモノマー及びグリコール酸、プロピオラクトン、γ−ブチロラクトン、δ−バレロラクトン、ε−カプロラクトン、トリメチレンカーボネート、p−ジオキサノン、テトラメチレンカーボネート、ε−ラクトン、1,5−ジオキセパン−2−オン又はそれらの混合物から選ばれるモノマーを含んでなるポリマーを示す]Polymer block B comprises trimethylene carbonate monomer and glycolic acid, propiolactone, γ-butyrolactone, δ-valerolactone, ε-caprolactone, trimethylene carbonate, p-dioxanone, tetramethylene carbonate, ε-lactone, 1,5 -Represents a polymer comprising a monomer selected from dioxepane-2-one or mixtures thereof]
のジブロックコポリマーであって、ジブロックコポリマーが50℃より低い温度で液体であることを特徴とするジブロックコポリマー。A diblock copolymer according to claim 1, wherein the diblock copolymer is a liquid at a temperature lower than 50 ° C.
a)1種もしくはそれより多いコポリマーを50℃より低い温度で水と混合し、
続いて
b)a)の下に得られるポリマー水溶液に、攪拌しながら活性成分を加える
ことを特徴とする方法。 A process for the preparation of an aqueous solution comprising an active ingredient and one or more diblock copolymers of the formula AB according to any one of claims 1 to 16 , comprising
a) mixing one or more copolymers with water at a temperature below 50 ° C .;
Subsequently, b) adding the active ingredient to the aqueous polymer solution obtained under a) with stirring.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US37790102P | 2002-05-03 | 2002-05-03 | |
PCT/EP2003/004368 WO2003093344A1 (en) | 2002-05-03 | 2003-04-24 | Polymeric microemulsions |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2005524730A JP2005524730A (en) | 2005-08-18 |
JP2005524730A5 true JP2005524730A5 (en) | 2006-06-08 |
JP4300184B2 JP4300184B2 (en) | 2009-07-22 |
Family
ID=29401581
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004501483A Expired - Fee Related JP4300184B2 (en) | 2002-05-03 | 2003-04-24 | Polymeric microemulsion |
Country Status (22)
Country | Link |
---|---|
US (3) | US20060034797A1 (en) |
EP (1) | EP1504047B1 (en) |
JP (1) | JP4300184B2 (en) |
KR (1) | KR20040111466A (en) |
CN (1) | CN1290893C (en) |
AR (1) | AR039522A1 (en) |
AT (1) | ATE380834T1 (en) |
AU (1) | AU2003222310B2 (en) |
BR (1) | BR0309688A (en) |
CA (1) | CA2483282C (en) |
DE (1) | DE60318035T2 (en) |
EA (1) | EA008244B1 (en) |
ES (1) | ES2298510T3 (en) |
IL (1) | IL164977A (en) |
MX (1) | MXPA04010778A (en) |
MY (1) | MY139066A (en) |
NO (1) | NO20045283L (en) |
NZ (1) | NZ536294A (en) |
PL (1) | PL220850B1 (en) |
TW (1) | TWI310388B (en) |
WO (1) | WO2003093344A1 (en) |
ZA (1) | ZA200408854B (en) |
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-
2003
- 2003-04-24 MX MXPA04010778A patent/MXPA04010778A/en active IP Right Grant
- 2003-04-24 KR KR10-2004-7015633A patent/KR20040111466A/en not_active Application Discontinuation
- 2003-04-24 AT AT03717321T patent/ATE380834T1/en not_active IP Right Cessation
- 2003-04-24 NZ NZ536294A patent/NZ536294A/en unknown
- 2003-04-24 BR BR0309688-2A patent/BR0309688A/en not_active IP Right Cessation
- 2003-04-24 ES ES03717321T patent/ES2298510T3/en not_active Expired - Lifetime
- 2003-04-24 AU AU2003222310A patent/AU2003222310B2/en not_active Ceased
- 2003-04-24 US US10/522,456 patent/US20060034797A1/en not_active Abandoned
- 2003-04-24 EP EP03717321A patent/EP1504047B1/en not_active Expired - Lifetime
- 2003-04-24 PL PL371934A patent/PL220850B1/en unknown
- 2003-04-24 WO PCT/EP2003/004368 patent/WO2003093344A1/en active IP Right Grant
- 2003-04-24 EA EA200401465A patent/EA008244B1/en not_active IP Right Cessation
- 2003-04-24 CA CA2483282A patent/CA2483282C/en not_active Expired - Fee Related
- 2003-04-24 DE DE60318035T patent/DE60318035T2/en not_active Expired - Lifetime
- 2003-04-24 JP JP2004501483A patent/JP4300184B2/en not_active Expired - Fee Related
- 2003-04-24 CN CNB038095793A patent/CN1290893C/en not_active Expired - Fee Related
- 2003-04-30 MY MYPI20031645A patent/MY139066A/en unknown
- 2003-05-02 AR ARP030101540A patent/AR039522A1/en unknown
- 2003-05-02 TW TW092112064A patent/TWI310388B/en active
-
2004
- 2004-11-02 ZA ZA200408854A patent/ZA200408854B/en unknown
- 2004-11-02 IL IL164977A patent/IL164977A/en active IP Right Grant
- 2004-12-02 NO NO20045283A patent/NO20045283L/en not_active Application Discontinuation
-
2011
- 2011-01-06 US US12/985,608 patent/US20110112115A1/en not_active Abandoned
-
2014
- 2014-12-01 US US14/557,058 patent/US20150086504A1/en not_active Abandoned
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